Dendrimeric tetravalent ligands for the serotonin-gated ion channel

Marco Paolino; Laura Mennuni; Germano Giuliani; Maurizio Anzini; Marco Lanza; Gianfranco Caselli; Chiara Galimberti; Maria Cristina Menziani; Alessandro Donati; Andrea Cappelli

doi:10.1039/C4CC02502D

Dendrimeric tetravalent ligands for the serotonin-gated ion channel†

Marco Paolino,^a Laura Mennuni,^b Germano Giuliani,^a Maurizio Anzini,^a Marco Lanza,^b Gianfranco Caselli,^b Chiara Galimberti,^b Maria Cristina Menziani,^c Alessandro Donati^a and Andrea Cappelli*^a

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^a Dipartimento di Biotecnologie, Chimica e Farmacia and European Research Centre for Drug Discovery and Development, Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy
E-mail: andrea.cappelli@unisi.it
Fax: +39 0577 234333
Tel: +39 0577 234320

^b Rottapharm Biotech S.r.l., Via Valosa di Sopra 3, 20900 Monza, Italy

^c Dipartimento di Scienze Chimiche e Geologiche, Università degli Studi di Modena e Reggio Emilia, Via Campi 183, 41100 Modena, Italy

Abstract

Multivalency is widely used in nature in specific recognition processes. This paper describes an approach to multivalency in the pentameric 5-HT₃ receptor, a ligand-gated ion channel, which constitutes an example of intrinsically multivalent biological receptors. Owing to the picomolar K_i value, TETRA-L represents an outstanding multivalent ligand for the neurotransmitter receptor.

Chemical Communications

Dendrimeric tetravalent ligands for the serotonin-gated ion channel†

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Dendrimeric tetravalent ligands for the serotonin-gated ion channel

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